Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents

As a continuation of our research and with the aim of obtaining new agents against Chagas disease, an extremely neglected disease which threatens 100 million people, eighteen new quinoxaline 1,4-di-Noxide derivatives have been synthesized following the Beirut reaction. The synthesis of the new deri...

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Main Authors: Pérez-Silanes, S. (Silvia), Monge, A. (Antonio), Aldana, I. (Ignacio), Gonzalez, M. (Mercedes), Cerecetto, H. (Hugo), Di-Maio, R. (Rossanna), Birriel, E. (Estefanía), Varela, J. (Javier), Arbillaga, L. (Leire), Azqueta, A. (Amaya), Crawford, P.W. (Philip W.), Devarapally, G. (Goutham), Galiano, S. (Silvia), Moreno-de-Viguri, E. (Elsa), Torres, E. (Enrique)
Format: info:eu-repo/semantics/article
Language:eng
Published: Elsevier 2014
Subjects:
Online Access:https://hdl.handle.net/10171/35794
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author Pérez-Silanes, S. (Silvia)
Monge, A. (Antonio)
Aldana, I. (Ignacio)
Gonzalez, M. (Mercedes)
Cerecetto, H. (Hugo)
Di-Maio, R. (Rossanna)
Birriel, E. (Estefanía)
Varela, J. (Javier)
Arbillaga, L. (Leire)
Azqueta, A. (Amaya)
Crawford, P.W. (Philip W.)
Devarapally, G. (Goutham)
Galiano, S. (Silvia)
Moreno-de-Viguri, E. (Elsa)
Torres, E. (Enrique)
author_facet Pérez-Silanes, S. (Silvia)
Monge, A. (Antonio)
Aldana, I. (Ignacio)
Gonzalez, M. (Mercedes)
Cerecetto, H. (Hugo)
Di-Maio, R. (Rossanna)
Birriel, E. (Estefanía)
Varela, J. (Javier)
Arbillaga, L. (Leire)
Azqueta, A. (Amaya)
Crawford, P.W. (Philip W.)
Devarapally, G. (Goutham)
Galiano, S. (Silvia)
Moreno-de-Viguri, E. (Elsa)
Torres, E. (Enrique)
author_sort Pérez-Silanes, S. (Silvia)
collection DSpace
description As a continuation of our research and with the aim of obtaining new agents against Chagas disease, an extremely neglected disease which threatens 100 million people, eighteen new quinoxaline 1,4-di-Noxide derivatives have been synthesized following the Beirut reaction. The synthesis of the new derivatives was optimized through the use of a new and more efficient microwave-assisted organic synthetic method. The new derivatives showed excellent in vitro biological activity against Trypanosoma cruzi. Compound 17, which was substituted with fluoro groups at the 6- and 7-positions of the quinoxaline ring, was the most active and selective in the cytotoxicity assay. The electrochemical study showed that the most active compounds, which were substituted by electron-withdrawing groups,possessed a greater ease of reduction of the N-oxide groups
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spelling oai:dadun.unav.edu:10171-357942020-03-04T02:37:54Z Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents Pérez-Silanes, S. (Silvia) Monge, A. (Antonio) Aldana, I. (Ignacio) Gonzalez, M. (Mercedes) Cerecetto, H. (Hugo) Di-Maio, R. (Rossanna) Birriel, E. (Estefanía) Varela, J. (Javier) Arbillaga, L. (Leire) Azqueta, A. (Amaya) Crawford, P.W. (Philip W.) Devarapally, G. (Goutham) Galiano, S. (Silvia) Moreno-de-Viguri, E. (Elsa) Torres, E. (Enrique) Reduction potential Cytotoxicity Mutagenicity Quinoxaline 1,4-di-N-oxide Trypanosoma cruzi Chagas disease As a continuation of our research and with the aim of obtaining new agents against Chagas disease, an extremely neglected disease which threatens 100 million people, eighteen new quinoxaline 1,4-di-Noxide derivatives have been synthesized following the Beirut reaction. The synthesis of the new derivatives was optimized through the use of a new and more efficient microwave-assisted organic synthetic method. The new derivatives showed excellent in vitro biological activity against Trypanosoma cruzi. Compound 17, which was substituted with fluoro groups at the 6- and 7-positions of the quinoxaline ring, was the most active and selective in the cytotoxicity assay. The electrochemical study showed that the most active compounds, which were substituted by electron-withdrawing groups,possessed a greater ease of reduction of the N-oxide groups 2014-04-13T11:45:35Z 2014-04-13T11:45:35Z 2013-05-30 info:eu-repo/semantics/article https://hdl.handle.net/10171/35794 eng FIMA (Fundación para la Investigación Médica Aplicada) from the University of Navarra. CSIC (Comisión de Investigación Científica) from Universidad de la República de Uruguay. Iberoamerican Program for Science and Technology (CYTED), network RIDIMEDCHAG. info:eu-repo/semantics/openAccess application/pdf Elsevier
spellingShingle Reduction potential
Cytotoxicity
Mutagenicity
Quinoxaline 1,4-di-N-oxide
Trypanosoma cruzi
Chagas disease
Pérez-Silanes, S. (Silvia)
Monge, A. (Antonio)
Aldana, I. (Ignacio)
Gonzalez, M. (Mercedes)
Cerecetto, H. (Hugo)
Di-Maio, R. (Rossanna)
Birriel, E. (Estefanía)
Varela, J. (Javier)
Arbillaga, L. (Leire)
Azqueta, A. (Amaya)
Crawford, P.W. (Philip W.)
Devarapally, G. (Goutham)
Galiano, S. (Silvia)
Moreno-de-Viguri, E. (Elsa)
Torres, E. (Enrique)
Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents
title Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents
title_full Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents
title_fullStr Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents
title_full_unstemmed Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents
title_short Novel quinoxaline 1,4-di-N-oxide derivatives as new potential antichagasic agents
title_sort novel quinoxaline 1,4-di-n-oxide derivatives as new potential antichagasic agents
topic Reduction potential
Cytotoxicity
Mutagenicity
Quinoxaline 1,4-di-N-oxide
Trypanosoma cruzi
Chagas disease
url https://hdl.handle.net/10171/35794
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